B-Raf
B-Raf is a serine/threonine protein kinase encoded by BRAF and functions as a central signal transducer in the RAS-RAF-MEK-ERK signaling cascade that regulates cell proliferation, differentiation, and survival[1][2]. Mechanistically, activated B-Raf phosphorylates MEK, leading to ERK activation and propagation of mitogenic signaling, making B-Raf a critical regulator of MAPK pathway output[2]. Dysregulation of this pathway is strongly linked to oncogenesis, and somatic BRAF mutations are among the most common kinase alterations identified in human cancer, particularly melanoma, colorectal cancer, thyroid cancer, and non-small-cell lung cancer[1][3]. In disease models, the canonical BRAF V600E mutation constitutively activates kinase signaling and promotes tumor cell growth independent of normal upstream regulatory inputs[2][3]. Compared with the related RAF isoforms A-Raf and C-Raf (RAF1), B-Raf displays stronger basal kinase activity and is the most potent activator of MEK-ERK signaling, making it a dominant MAPK pathway driver in many BRAF-mutant tumors[2]. For experimental applications, selective B-Raf inhibitors have been widely used to suppress oncogenic MAPK signaling and to investigate pathway dependence in cancer models[4]. The development of mutation-selective inhibitors, including compounds targeting BRAF V600E, established B-Raf as a validated therapeutic and mechanistic target and continues to support research on signaling regulation, drug resistance, and combination treatment strategies[4][5].
References:
- [1]. Davies H, et al. Mutations of the BRAF gene in human cancer. Nature. 2002 Jun 27;417(6892):949-54. [Content Brief]
- [2]. Wan PT, et al. Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell. 2004 Mar 19;116(6):855-67. [Content Brief]
- [3]. B-Raf gene information from NCBI.
- [4]. Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6. [Content Brief]
- [5]. Bollag G, et al. Vemurafenib: the first drug approved for BRAF-mutant cancer. Nat Rev Drug Discov. 2012 Nov;11(11):873-86. [Content Brief]
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B-Raf 관련 제품 (97)
관련 제품 (97)
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Antibodies (3)
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BRAFV600E-IN-2
0 ImagesCat. No.: HY-175831CAS No.: 3027070-47-6BRAFV600E-IN-2 is a BRAF V600E inhibitor with IC50 ≤10 nM. BRAFV600E-IN-2 has anti-tumor activity.
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EGFR/BRAFV600E-IN-2
0 ImagesCat. No.: HY-149517EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAFV600E, and EGFRT790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency.
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Sorafenib-d3 tosylate
0 ImagesCat. No.: HY-10201S4CAS No.: 1333386-17-6Synonyms: Donafenib tosylate; Bay 43-9006-d3 tosylateSorafenib-d3 (Donafenib) tosylate is the deuterated-labeled Sorafenib tosylate (HY-10201A). Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
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B-Raf IN 9
0 ImagesCat. No.: HY-147854CAS No.: 2477725-18-9
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CST905
0 ImagesCat. No.: HY-175435CAS No.: 3094183-98-6CST905 is a potent BRAF-V600E PROTAC degrader with a DC50 of 18 nM. CST905 recruits the VHL E3 ligase to form a ternary complex, mediating the degradation of BRAF-V600E via the ubiquitin-proteasome pathway. The ligand of CST905 disrupts the RAF dimerization interface, thereby preventing the aberrant activation of the harmful MAPK/ERK pathway in RAS-mutated cells while degrading the target protein. CST905 can be used in studies related to malignant melanoma and neuroblastoma.
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B-Raf IN 7
0 ImagesCat. No.: HY-147852CAS No.: 2477725-07-6B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor, with an IC50 of 110.23 nM. B-Raf IN 7 exhibits antitumor activity against colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela) and human prostate cancer (PC-3) cells, with IC50 values of 7.50, 9.87, 10.57, 11.63 and 12.83 µM.
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CDC20/HSP90-IN-1
0 ImagesCat. No.: HY-179012CDC20/HSP90-IN-1 (Compound 2b) is a Cdc20/Hsp90 inhibitor with a Kd of 16.2 μM for Cdc20 and a Kd of 0.241 μM for Hsp90α. CDC20/HSP90-IN-1 exerts potent antitumor activity through reducing p53-mediated Cdc20, upregulating Bim, downregulating Cyclin B1 expression, and disturbing B-Raf and AKT pathways via destroying Hsp90 chaperone function. CDC20/HSP90-IN-1 overcomes Vemurafenib (HY-12057)-induced resistant melanoma.
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MEK/RAF-IN-1
0 ImagesCat. No.: HY-162873MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer.
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ARQ-736
0 ImagesCat. No.: HY-16063CAS No.: 1228237-57-7
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Takeda-6D
0 ImagesTakeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity.
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SB-590885 (GMP)
0 ImagesCat. No.: HY-10966GCAS No.: 405554-55-4SB-590885 GMP is SB-590885 (HY-10966) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SB-590885 is a BRAF/c-Raf kinase inhibitor that selectively targets B-Raf, and it amplifies the ERK/MAPK signaling pathway in RAS-activated cells. SB-590885 effectively inhibits the malignant proliferation, transformation and tumorigenicity of oncogenic B-Raf cells; it also induces the proliferation of erythroid progenitor cells, delays their differentiation and promotes hemoglobin synthesis, thereby improving ineffective erythropoiesis and reducing apoptosis. SB-590885 exerts a synergistic effect with TGF-β inhibitors and glucocorticoids, significantly promoting the formation of erythroid colonies in cells from patients with Diamond-Blackfan anemia (DBA). SB-590885 is mainly used in relevant studies on DBA, cisplatin-induced myelosuppression-related anemia, and pan-cancers such as melanoma and colorectal cancer.
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BRAF ligand-2
0 ImagesCat. No.: HY-187012CAS No.: 2882167-76-0BRAF ligand-2 is a BRAF ligand that can be used to synthesize PROTACs, such as Tagarafdeg (HY-153341).
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COX/5-LO-IN-2
0 ImagesCat. No.: HY-181061COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC50 of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer.
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EGFR/BRAFV600E-IN-6
0 ImagesCat. No.: HY-180154CAS No.: 3120155-78-1EGFR/BRAFV600E-IN-6 (Compound 7c) is a dual EGFR/BRAFV600E inhibitor with IC50 values of 0.12 and 0.05 μM. EGFR/BRAFV600E-IN-6 can activate caspase-3/8/9, unregulate Bax expression and downregulate Bcl-2 levels. EGFR/BRAFV600E-IN-6 can induce apoptosis and shows antioxidant activity. EGFR/BRAFV600E-IN-6 can be used for the research of cancer, such as colon cancer.
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RAF-IN-1
0 ImagesCat. No.: HY-144271CAS No.: 2695505-82-7
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Multi-target kinase-IN-8
0 ImagesCat. No.: HY-179098Multi-target kinase-IN-8 (3d) is an anti-cancer agent. Multi-target kinase-IN-8 exhibits inhibitory activity against various protein kinases (B-Raf V600E (IC50 = 0.078 µg/mL), c-Met (IC50 = 0.405 µg/mL), Pim-1 (IC50 = 1.053 µg/mL), EGFR WT (IC50 = 0.177 µg/mL), VEGFR-2 (IC50 = 0.275 µg/mL)). Multi-target kinase-IN-8 can induce cell cycle arrest and promote early and late apoptosis. Multi-target kinase-IN-8 is commonly used in cancer research.
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Multi-kinase-IN-5
0 ImagesCat. No.: HY-149415Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC50 of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively.
